It is well recognised that in therapy one is always looking for a balance between the curing effect of a pharmaceutically active compound and the detrimental side effects the active compound may exert. From this point of view, it is of prime concern not to use more of an active compound then necessary and not to use it for a longer period than required. At the same time, there is the challenge of the effective delivery of a pharmaceutically active compound to an active site and of achieving an acceptable rate of release of the pharmaceutically active compound. These issues have our constant attention in developing and improving pharmaceutical therapies.
Many approaches have been adopted to attempt to deal with these issues. For example, a particularly high dose of a pharmaceutically active compound may be administered to ensure that at least an effective amount of it reaches the desired site of treatment. This approach to administration is clearly problematic, because at high dose the pharmaceutically active compound may exerts its detrimental effects. For example, see Horstick et al (2001) Circulation 104:3125. They describe how C1INH significantly protects ischemic tissue from reperfusion damage at 40 IU/kg, but provokes detrimental effects at overly high doses (a dose of 100 IU/kg or more).
There remains a need for methods for delivering a pharmaceutically active compound with maximum effectiveness. This method should allow for the administration of a patient's dose requirement of optimal effectivity, while minimising undesirable side effects.